AU2009260782B2 - Thiophene or thiazole derivatives and their use as PI3K inhibitors - Google Patents

Thiophene or thiazole derivatives and their use as PI3K inhibitors Download PDF

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Publication number
AU2009260782B2
AU2009260782B2 AU2009260782A AU2009260782A AU2009260782B2 AU 2009260782 B2 AU2009260782 B2 AU 2009260782B2 AU 2009260782 A AU2009260782 A AU 2009260782A AU 2009260782 A AU2009260782 A AU 2009260782A AU 2009260782 B2 AU2009260782 B2 AU 2009260782B2
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AU
Australia
Prior art keywords
membered
nitrogen
optionally substituted
sulfur
oxygen
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
AU2009260782A
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English (en)
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AU2009260782A1 (en
Inventor
David P. Cardin
Jeffrey L. Gaulin
Paul D. Greenspan
Christelle C. Renou
Stepan Vyskocil
Tianlin Xu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Millennium Pharmaceuticals Inc
Original Assignee
Millennium Pharmaceuticals Inc
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41010579&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2009260782(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Millennium Pharmaceuticals Inc filed Critical Millennium Pharmaceuticals Inc
Publication of AU2009260782A1 publication Critical patent/AU2009260782A1/en
Priority to AU2013203960A priority Critical patent/AU2013203960A1/en
Application granted granted Critical
Publication of AU2009260782B2 publication Critical patent/AU2009260782B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2009260782A 2008-06-19 2009-06-17 Thiophene or thiazole derivatives and their use as PI3K inhibitors Ceased AU2009260782B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2013203960A AU2013203960A1 (en) 2008-06-19 2013-04-11 Thiophene or thiazole derivatives and their use as PI3K inhibitors

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13248408P 2008-06-19 2008-06-19
US61/132,484 2008-06-19
PCT/US2009/003607 WO2009154741A1 (en) 2008-06-19 2009-06-17 Thiophene or thiazole derivatives and their use as pi3k inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2013203960A Division AU2013203960A1 (en) 2008-06-19 2013-04-11 Thiophene or thiazole derivatives and their use as PI3K inhibitors

Publications (2)

Publication Number Publication Date
AU2009260782A1 AU2009260782A1 (en) 2009-12-23
AU2009260782B2 true AU2009260782B2 (en) 2014-12-11

Family

ID=41010579

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009260782A Ceased AU2009260782B2 (en) 2008-06-19 2009-06-17 Thiophene or thiazole derivatives and their use as PI3K inhibitors

Country Status (21)

Country Link
US (3) US8183240B2 (enExample)
EP (1) EP2313399B1 (enExample)
JP (1) JP5596026B2 (enExample)
KR (1) KR20110018451A (enExample)
CN (1) CN102066365A (enExample)
AU (1) AU2009260782B2 (enExample)
BR (1) BRPI0914223A2 (enExample)
CA (1) CA2727069A1 (enExample)
CL (1) CL2010001474A1 (enExample)
CO (1) CO6331431A2 (enExample)
CR (1) CR20110032A (enExample)
EA (1) EA201170052A1 (enExample)
ES (1) ES2491522T3 (enExample)
GE (1) GEP20125650B (enExample)
IL (1) IL210055A0 (enExample)
MA (1) MA32468B1 (enExample)
MX (1) MX2010014125A (enExample)
NZ (1) NZ589844A (enExample)
UA (1) UA106206C2 (enExample)
WO (1) WO2009154741A1 (enExample)
ZA (1) ZA201008875B (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9029411B2 (en) 2008-01-25 2015-05-12 Millennium Pharmaceuticals, Inc. Thiophenes and uses thereof
CN102066365A (zh) * 2008-06-19 2011-05-18 米伦纽姆医药公司 噻吩或噻唑衍生物和其作为pi3k抑制剂的用途
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9139589B2 (en) 2009-01-30 2015-09-22 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
JP2013533318A (ja) * 2010-08-11 2013-08-22 ミレニアム ファーマシューティカルズ， インコーポレイテッド ヘテロアリールおよびその使用
MA34797B1 (fr) * 2010-08-11 2014-01-02 Millennium Pharm Inc Hétéroaryles et leurs utilisations
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
JP5726635B2 (ja) 2010-08-25 2015-06-03 株式会社Ｎｔｔドコモ マルチモードフロントエンド回路
PH12013500723A1 (en) 2010-10-13 2017-08-23 Millennium Pharm Inc Heteroaryls and uses thereof
CN102503930B (zh) * 2011-10-28 2014-07-02 浙江大学 3,4,5,-三取代氨基噻吩类化合物及其制备和用途
CA2857302C (en) 2011-12-15 2020-08-25 Novartis Ag Use of inhibitors of the activity or function of pi3k
US20130165472A1 (en) * 2011-12-23 2013-06-27 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
IN2014DN06898A (enExample) 2012-03-14 2015-05-15 Salk Inst For Biological Studi
CA2903582C (en) 2013-03-14 2021-06-08 Salk Institute For Biological Studies Oncolytic adenovirus compositions
MX2015011899A (es) 2013-03-15 2016-05-05 Genentech Inc Metodos para el tratamiento de cáncer y prevención de resistencia a los fármacos para el cáncer.
KR20160115999A (ko) * 2014-02-14 2016-10-06 더 유니버시티 오브 브리티쉬 콜롬비아 치료제로서의 인간 안드로겐 수용체 dna-결합 도메인(dbd) 화합물 및 그의 사용 방법
JP7015551B2 (ja) 2016-02-23 2022-02-15 ソーク インスティテュート フォー バイオロジカル スタディーズ ウイルス動態への影響を最小限にするための治療用アデノウイルスにおける外因性遺伝子発現
WO2017147265A1 (en) 2016-02-23 2017-08-31 Salk Institute For Biological Studies High throughput assay for measuring adenovirus replication kinetics
CA3045892A1 (en) 2016-12-12 2018-06-21 Salk Institute For Biological Studies Tumor-targeting synthetic adenoviruses and uses thereof
BR112020019942A2 (pt) 2018-04-09 2021-01-26 Salk Institute For Biological Studies composições de adenovírus oncolítico com propriedades de replicação aprimoradas
US20220363673A1 (en) * 2019-06-28 2022-11-17 Pfizer Inc. 5-(Thiophen-2-YL)-1 H-Tetrazole Derivative as BCKDK Inhibitors Useful for Treating Various Diseases
CN110759900B (zh) * 2019-10-25 2021-07-30 沈阳药科大学 噻吩类化合物的制备方法和用途
EP4285723A3 (en) 2019-12-20 2024-03-27 Bayer Aktiengesellschaft Substituted thiophene carboxamides, thiophene carboxylic acids and derivatives thereof
CN113527281B (zh) * 2020-04-20 2023-12-22 昆山彭济凯丰生物科技有限公司 杂环化合物及其制备方法和应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007129044A1 (en) * 2006-05-03 2007-11-15 Astrazeneca Ab Thiazole derivatives and their use as anti-tumour agents
WO2008023159A1 (en) * 2006-08-24 2008-02-28 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
WO2009042607A1 (en) * 2007-09-24 2009-04-02 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
WO2009094224A1 (en) * 2008-01-25 2009-07-30 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD275870A1 (de) 1988-09-27 1990-02-07 Univ Leipzig Verfahren zur herstellung von in 5-position verschiedenartig substituierten 3-aminothiophen-4-carbonitrilen
EP1742627A4 (en) 2004-05-06 2009-08-26 Plexxikon Inc PDE4B HEMMER AND ITS USE
GB0508472D0 (en) * 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
UA95799C2 (en) 2006-04-26 2011-09-12 Ф. Хоффманн-Ля Рош Аг Pharmaceutical compounds
CN102066365A (zh) * 2008-06-19 2011-05-18 米伦纽姆医药公司 噻吩或噻唑衍生物和其作为pi3k抑制剂的用途

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007129044A1 (en) * 2006-05-03 2007-11-15 Astrazeneca Ab Thiazole derivatives and their use as anti-tumour agents
WO2008023159A1 (en) * 2006-08-24 2008-02-28 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
WO2009042607A1 (en) * 2007-09-24 2009-04-02 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
WO2009094224A1 (en) * 2008-01-25 2009-07-30 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors

Also Published As

Publication number Publication date
CO6331431A2 (es) 2011-10-20
NZ589844A (en) 2012-11-30
UA106206C2 (ru) 2014-08-11
US8183240B2 (en) 2012-05-22
ES2491522T3 (es) 2014-09-08
JP5596026B2 (ja) 2014-09-24
EP2313399A1 (en) 2011-04-27
EA201170052A1 (ru) 2011-06-30
WO2009154741A8 (en) 2010-03-25
MX2010014125A (es) 2011-02-24
EP2313399B1 (en) 2014-05-28
AU2009260782A1 (en) 2009-12-23
JP2011524904A (ja) 2011-09-08
KR20110018451A (ko) 2011-02-23
CL2010001474A1 (es) 2011-04-29
CA2727069A1 (en) 2009-12-23
US20130217689A1 (en) 2013-08-22
IL210055A0 (en) 2011-02-28
BRPI0914223A2 (pt) 2019-09-24
ZA201008875B (en) 2012-02-29
US20120202812A1 (en) 2012-08-09
US20100075951A1 (en) 2010-03-25
CR20110032A (es) 2011-03-14
CN102066365A (zh) 2011-05-18
MA32468B1 (fr) 2011-07-03
US8440664B2 (en) 2013-05-14
GEP20125650B (en) 2012-09-25
WO2009154741A1 (en) 2009-12-23

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Legal Events

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DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ XU, TIANLIN; CARDIN, DAVID P.; GREENSPAN, PAUL D.; RENOU, CHRISTELLE C.; VYSKOCIL, STEPAN AND GAULIN, JEFFREY L.

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired